Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. Azatadine puts back the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. It protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice. Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 90 mg/mL|
The pharmacology of azatadine, a potential antiallergy drug.
Tozzi S,et al. Agents Actions. 1974 Oct;4(4):264-70. PMID: 4155594.
Comparative effects of loratadine and azatadine in the treatment of seasonal allergic rhinitis.
Katelaris C. Asian Pac J Allergy Immunol. 1990 Dec;8(2):103-7. PMID: 1982614.
|Related Histamine Receptor Products|
Fexofenadine is a nonsedating antihistamine drug which is indicated for treatment of seasonal allergic rhinitis.
|Roxatidine Acetate HCl
Roxatidine Acetate HCl is a specific and competitive histamin H2-receptor antagonist, with IC50 of 3.2 μM, inhibits gastric acid secretion and ulcer formation.
Ranitidine is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers.
Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.
Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
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